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World class computing and information science research at Strathclyde...

The Strathprints institutional repository is a digital archive of University of Strathclyde's Open Access research outputs. Strathprints provides access to thousands of Open Access research papers by University of Strathclyde researchers, including by researchers from the Department of Computer & Information Sciences involved in mathematically structured programming, similarity and metric search, computer security, software systems, combinatronics and digital health.

The Department also includes the iSchool Research Group, which performs leading research into socio-technical phenomena and topics such as information retrieval and information seeking behaviour.

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Distamycin Analogues with Enhanced Lipophilicity: Synthesis and Antimicrobial Activity

Khalaf, A.I. and Waigh, R.D. and Drummond, A.J. and Pringle, B. and McGroarty, I. and Skellern, G.G. and Suckling, C.J. (2004) Distamycin Analogues with Enhanced Lipophilicity: Synthesis and Antimicrobial Activity. Journal of Medicinal Chemistry, 47 (8). pp. 2133-2156. ISSN 0022-2623

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Abstract

Forty-eight heterocyclic amino acid trimers, analogues of distamycin, with a number of features that enhance lipophilicity are described. They contain alkyl or cycloalkyl groups larger than methyl; some are N-terminated by acetamide or methoxybenzamide and are C-terminated by dimethylaminopropyl or aliphatic heterocylic aminopropyl substituents. The ability of these compounds to bind principally to AT tracts of DNA has been evaluated using capillary zone electrophoresis. Significant antimicrobial activity against key organisms such as MRSA and Candida albicans is shown by several compounds, especially those containing a thiazole. Moreover, these compounds have low toxicity with respect to several mammalian cell lines.